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Radiotracers for positron emission tomography (PET) targeting tumour-associated carbonic anhydrase isoforms
European Journal of Medicinal Chemistry ( IF 6.0 ) Pub Date : 2020-11-25 , DOI: 10.1016/j.ejmech.2020.113046
Valeria Burianova , Stanislav Kalinin , Claudiu T. Supuran , Mikhail Krasavin

The tumour-associated, cell membrane-bound isoforms IX and XII of human carbonic anhydrase (CA, EC 4.2.1.1) are overexpressed in cancer cells contributing to the hypoxic tumour pH/metabolism regulating machinery and as thus, can serve as markers of neoplastic tissue. Inhibitors of CAs can be employed both for the treatment of hypoxic tumours and in the design of radiotracers for positron emission tomography and imaging of such cancers. The present review provides a comprehensive summary of the progress achieved to-date in the field of developing PET-tracers based on monoclonal antibodies, biomolecules, and small-molecule ligands of CA IX and XII.



中文翻译:

靶向肿瘤相关碳酸酐酶同工型的正电子发射断层扫描(PET)的放射性示踪剂

人碳酸酐酶与肿瘤相关的细胞膜结合同工型IX和XII(CA,EC 4.2.1.1)在癌细胞中过表达,这有助于缺氧性肿瘤的pH /代谢调节机制,因此可以用作赘生物的标志物组织。CA抑制剂既可用于治疗低氧性肿瘤,也可用于放射示踪剂的设计,以进行正电子发射断层扫描和此类癌症的成像。本综述提供了迄今为止在基于CA IX和XII的单克隆抗体,生物分子和小分子配体的PET示踪剂开发领域取得的进展的全面总结。

更新日期:2020-11-26
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